Target
Hydroxycarboxylic acid receptor 2
Ligand
BDBM50297999
Substrate
n/a
Meas. Tech.
ChEMBL_585074 (CHEMBL1054340)
EC50
1300±n/a nM
Citation
 Schmidt, DSmenton, ARaghavan, SCarballo-Jane, ELubell, SCiecko, THolt, TGWolff, MTaggart, AWilsie, LKrsmanovic, MRen, NBlom, DCheng, KMcCann, PEGerard Waters, MTata, JColletti, S Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia. Bioorg Med Chem Lett 19:4768-72 (2009) [PubMed]  Article 
Target
Name:
Hydroxycarboxylic acid receptor 2
Synonyms:
G-protein coupled receptor 109A | G-protein coupled receptor HM74A | GPR109A | HCA2 | HCAR2 | HCAR2_HUMAN | HM74A | Hydroxycarboxylic acid receptor 2 | NIACR1 | Niacin Receptor GPR109A | Nicotinic acid receptor 1
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
41868.22
Organism:
Homo sapiens (Human)
Description:
Membranes from CHO cells expressing the recombinant human GPR109A were used in competition binding assay.
Residue:
363
Sequence:
MNRHHLQDHFLEIDKKNCCVFRDDFIVKVLPPVLGLEFIFGLLGNGLALWIFCFHLKSWKSSRIFLFNLAVADFLLIICLPFLMDNYVRRWDWKFGDIPCRLMLFMLAMNRQGSIIFLTVVAVDRYFRVVHPHHALNKISNRTAAIISCLLWGITIGLTVHLLKKKMPIQNGGANLCSSFSICHTFQWHEAMFLLEFFLPLGIILFCSARIIWSLRQRQMDRHAKIKRAITFIMVVAIVFVICFLPSVVVRIRIFWLLHTSGTQNCEVYRSVDLAFFITLSFTYMNSMLDPVVYYFSSPSFPNFFSTLINRCLQRKMTGEPDNNRSTSVELTGDPNKTRGAPEALMANSGEPWSPSYLGPTSP
  
Inhibitor
Name:
BDBM50297999
Synonyms:
(+/-)-5-(2,5-difluorophenyl)-4,5,6,7-tetrahydro-1H-indazole-3-carboxylic acid | 5-(2,5-difluorophenyl)-4,5,6,7-tetrahydro-1H-indazole-3-carboxylic acid, hydrobromide | 5-(2,5-difluorophenyl)-4,5,6,7-tetrahydro-1H-indazole-3-carboxylic acid, hydrochloride | CHEMBL1237148 | CHEMBL542000
Type:
Small organic molecule
Emp. Form.:
C14H12F2N2O2
Mol. Mass.:
278.2541
SMILES:
OC(=O)c1n[nH]c2CCC(Cc12)c1cc(F)ccc1F
Structure:
Search PDB for entries with ligand similarity: